Formulation and evaluation of fast dissolving tablet containing vilazodone nanocrystals for solubility and dissolution enhancement using soluplus: In vitro-In vivo Study

Abstract

A major problem in the development of an efficacious formulation of the drug is its pitiable aqueous solubility which affects stability and bioavailability of drug formulation. There is a need for systematic formulation approaches to make poorly soluble drugs bioavailable. The present investigation aims to increase solubility and dissolution of Vilazodone (VLZ) an antidepressant drug by preparing its nanoparticles using graft copolymer Soluplus and polyvinylpyrrolidone K-30 (PVP K 30) by evaporative precipitation into aqueous solution method. The prepared nanoparticles were characterized by FTIR, DSC, XRD, SEM, Particle size by DLS and saturation solubility. The nanoparticles showed a remarkable increase in the aqueous saturation solubility i.e., NP1, NP2, NP3 and NP4 shows 4.4, 4.6, 7.7 and 7.8 folds respectively increase in aqueous solubility as compared to VLZ. The nanoparticles NP4 batch with the highest solubility is converted into fast dissolving tablet. The tablets were evaluated for different parameters and found to possess more dissolution (89.386% release) as compared to pure drug (51.652%). The rise in solubility and dissolution may be due to either reduction in particle size leads to increase surface area or micelles formation due to Soluplus and reduction in crystallinity of drug. In vivo study reveals that optimized Vilazodone nanoparticles (VLZNP) elicited significant antidepressant-like activity.